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硫代秋水仙碱衍生物及其在 CEM 细胞治疗中的 19F 磁共振体外应用。

Derivatives of thiocolchicine and its applications to CEM cells treatment using 19F magnetic resonance ex vivo.

机构信息

National Research Council Canada, Institute for Biodiagnostics (West), 3330 Hospital Drive NW, Calgary, Alberta, Canada T2N 4N1.

出版信息

Bioorg Chem. 2010 Feb;38(1):1-6. doi: 10.1016/j.bioorg.2009.10.002. Epub 2009 Nov 1.

Abstract

It was shown, that cultured ex vivo human T-Lymphoblastoid (CEM) cells respond to synthesized thiocolchicine and fluorine thiocolchicine derivatives. The preparation of derivatives with substitution at C-3 and C-7 is described. All compounds were used at concentration from 1 nM to 1000 nM. Inhibitory effects of these compounds were examined in the three-dimensional (3-D) culture and cells morphology during treatment was monitored using 9.4 T MRI system. We performed studies of these compounds in CEM cells ex vivo using 1H and 19F Magnetic Resonance Imaging (MRI), 19F Magnetic Resonance Spectroscopy (MRS), High Performance Liquid Chromatography coupled with Ultra Violet (HPLC-UV) and Electron Impact Mass Spectrometry (EIMS). The results of the multi-technique approach are consistent with the fact that the new derivatives are more efficient than colchicine and thiocolchicine ex vivo.

摘要

研究表明,体外培养的人 T 淋巴细胞白血病细胞(CEM)对合成的硫代秋水仙碱和氟代硫代秋水仙碱衍生物有反应。本文描述了 C-3 和 C-7 取代的衍生物的制备。所有化合物均在 1 nM 至 1000 nM 的浓度下使用。在三维(3-D)培养中检查了这些化合物的抑制作用,并使用 9.4 T MRI 系统监测治疗过程中的细胞形态。我们使用 1H 和 19F 磁共振成像(MRI)、19F 磁共振波谱(MRS)、高效液相色谱-紫外(HPLC-UV)和电子冲击质谱(EIMS)对 CEM 细胞进行了这些化合物的体外研究。多技术方法的结果与以下事实一致,即新的衍生物在体外比秋水仙碱和硫代秋水仙碱更有效。

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